Comperative pharmacokinetic and pharmacodynamic characteristics of amlodipine besylate and amlodipine nicotinate in healthy subjects

Ji-Young Park, K. A. Kim, P. W. Park, O. J. Lee, J. S. Kim, G. H. Lee, M. C. Ha, J. H. Park, M. J. O, J. H. Ryu

Research output: Contribution to journalArticle

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Abstract

Background and aim: Amlodipine, a dihydropyridine calcium antagonist, is prescribed for the management of angina and hypertension, and is sold as amlodipine besylate. However, a new salt formulation, amlodipine nicotinate, has recently been developed. Here, we evaluated the comparative pharmacokinetic and pharmacodynamic characteristics of the nicotinate and besylate forms of amlodipine. Subjects and methods: A randomized, 2-way crossover study was conducted in 18 healthy male volunteers to compare the pharmacokinetics and pharmacodynamics of these two forms, i.e. amlodipine nicotinate (test) and amlodipine besylate (reference), after administration of a single dose of 5 mg of each drug and a washout period between doses of 4 weeks. Blood samples for the pharmacokinetic analysis of amlodipine were obtained over the 144-hour period after administration. Systolic and diastolic blood pressures and pulse rates were recorded immediately prior to each blood sampling. Results: All participants completed both treatment periods, and no serious adverse events occurred during the study period. After administering a single dose of each formulation, mean AUC0-∞ and Cmax values were 190.91 ± 60.49 ng × h/ml and 3.87 ± 1.04 ng/ml for the test formulation and 203.15 ± 52.05 ng × h/ml and 4.01 ± 0.60 ng/ml for the reference formulation, respectively. The 90% confidence intervals of test/reference mean ratios for AUC0-∞ and Cmax fell within the predetermined equivalence range of 80 - 125%. Pharmacodynamic profiles including systolic and diastolic blood pressures and pulse rates exhibited no significant differences between the two formulations. Conclusion: The two amlodipine formulations showed similar pharmacokinetic and pharmacodynamic characteristics and the new amlodipine formulation, amlodipine nicotinate, was found to be equivalent for pharmacokinetics to the currently available amlodipine besylate with respect to the rate and extent of amlodipine absorption.

Original languageEnglish
Pages (from-to)641-647
Number of pages7
JournalInternational Journal of Clinical Pharmacology and Therapeutics
Volume44
Issue number12
Publication statusPublished - 2006 Dec 1

Fingerprint

Amlodipine
Healthy Volunteers
Pharmacokinetics
Blood Pressure
Heart Rate
amlodipine nicotinate
Niacin
Cross-Over Studies
Salts
Confidence Intervals
Hypertension
Calcium

Keywords

  • Amlodipine
  • Bioavailability
  • Pharmacodynamics
  • Pharmacokinetics
  • Salt substitution

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

Comperative pharmacokinetic and pharmacodynamic characteristics of amlodipine besylate and amlodipine nicotinate in healthy subjects. / Park, Ji-Young; Kim, K. A.; Park, P. W.; Lee, O. J.; Kim, J. S.; Lee, G. H.; Ha, M. C.; Park, J. H.; O, M. J.; Ryu, J. H.

In: International Journal of Clinical Pharmacology and Therapeutics, Vol. 44, No. 12, 01.12.2006, p. 641-647.

Research output: Contribution to journalArticle

Park, Ji-Young ; Kim, K. A. ; Park, P. W. ; Lee, O. J. ; Kim, J. S. ; Lee, G. H. ; Ha, M. C. ; Park, J. H. ; O, M. J. ; Ryu, J. H. / Comperative pharmacokinetic and pharmacodynamic characteristics of amlodipine besylate and amlodipine nicotinate in healthy subjects. In: International Journal of Clinical Pharmacology and Therapeutics. 2006 ; Vol. 44, No. 12. pp. 641-647.
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AU - Park, Ji-Young

AU - Kim, K. A.

AU - Park, P. W.

AU - Lee, O. J.

AU - Kim, J. S.

AU - Lee, G. H.

AU - Ha, M. C.

AU - Park, J. H.

AU - O, M. J.

AU - Ryu, J. H.

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N2 - Background and aim: Amlodipine, a dihydropyridine calcium antagonist, is prescribed for the management of angina and hypertension, and is sold as amlodipine besylate. However, a new salt formulation, amlodipine nicotinate, has recently been developed. Here, we evaluated the comparative pharmacokinetic and pharmacodynamic characteristics of the nicotinate and besylate forms of amlodipine. Subjects and methods: A randomized, 2-way crossover study was conducted in 18 healthy male volunteers to compare the pharmacokinetics and pharmacodynamics of these two forms, i.e. amlodipine nicotinate (test) and amlodipine besylate (reference), after administration of a single dose of 5 mg of each drug and a washout period between doses of 4 weeks. Blood samples for the pharmacokinetic analysis of amlodipine were obtained over the 144-hour period after administration. Systolic and diastolic blood pressures and pulse rates were recorded immediately prior to each blood sampling. Results: All participants completed both treatment periods, and no serious adverse events occurred during the study period. After administering a single dose of each formulation, mean AUC0-∞ and Cmax values were 190.91 ± 60.49 ng × h/ml and 3.87 ± 1.04 ng/ml for the test formulation and 203.15 ± 52.05 ng × h/ml and 4.01 ± 0.60 ng/ml for the reference formulation, respectively. The 90% confidence intervals of test/reference mean ratios for AUC0-∞ and Cmax fell within the predetermined equivalence range of 80 - 125%. Pharmacodynamic profiles including systolic and diastolic blood pressures and pulse rates exhibited no significant differences between the two formulations. Conclusion: The two amlodipine formulations showed similar pharmacokinetic and pharmacodynamic characteristics and the new amlodipine formulation, amlodipine nicotinate, was found to be equivalent for pharmacokinetics to the currently available amlodipine besylate with respect to the rate and extent of amlodipine absorption.

AB - Background and aim: Amlodipine, a dihydropyridine calcium antagonist, is prescribed for the management of angina and hypertension, and is sold as amlodipine besylate. However, a new salt formulation, amlodipine nicotinate, has recently been developed. Here, we evaluated the comparative pharmacokinetic and pharmacodynamic characteristics of the nicotinate and besylate forms of amlodipine. Subjects and methods: A randomized, 2-way crossover study was conducted in 18 healthy male volunteers to compare the pharmacokinetics and pharmacodynamics of these two forms, i.e. amlodipine nicotinate (test) and amlodipine besylate (reference), after administration of a single dose of 5 mg of each drug and a washout period between doses of 4 weeks. Blood samples for the pharmacokinetic analysis of amlodipine were obtained over the 144-hour period after administration. Systolic and diastolic blood pressures and pulse rates were recorded immediately prior to each blood sampling. Results: All participants completed both treatment periods, and no serious adverse events occurred during the study period. After administering a single dose of each formulation, mean AUC0-∞ and Cmax values were 190.91 ± 60.49 ng × h/ml and 3.87 ± 1.04 ng/ml for the test formulation and 203.15 ± 52.05 ng × h/ml and 4.01 ± 0.60 ng/ml for the reference formulation, respectively. The 90% confidence intervals of test/reference mean ratios for AUC0-∞ and Cmax fell within the predetermined equivalence range of 80 - 125%. Pharmacodynamic profiles including systolic and diastolic blood pressures and pulse rates exhibited no significant differences between the two formulations. Conclusion: The two amlodipine formulations showed similar pharmacokinetic and pharmacodynamic characteristics and the new amlodipine formulation, amlodipine nicotinate, was found to be equivalent for pharmacokinetics to the currently available amlodipine besylate with respect to the rate and extent of amlodipine absorption.

KW - Amlodipine

KW - Bioavailability

KW - Pharmacodynamics

KW - Pharmacokinetics

KW - Salt substitution

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